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Current Drug Delivery
ISSN (Print): 1567-2018
ISSN (Online): 1875-5704
DOI: 10.2174/1567201811666140414113838      Price:  $58

Formulation and Evaluation of Gastroretentive Microballoons Containing Baclofen for a Floating Oral Controlled Drug Delivery System

Author(s): T.S. Dube, N.S. Ranpise and A.N. Ranade
Pages 805-816 (12)
The objective of the present study was to fabricate and evaluate a multiparticulate oral gastroretentive dosage form of baclofen characterized by a central large cavity (hollow core) promoting unmitigated floatation with practical applications to alleviate the signs and symptoms of spasticity and muscular rigidity. Solvent diffusion and evaporation procedure were applied to prepare floating microspheres with a central large cavity using various combinations of ethylcellulose (release retardant) and HPMC K4M (release modifier) dissolved in a mixture of dichloromethane and methanol (2:1). The obtained microspheres (700-1000 µm) exhibit excellent floating ability (86±2.00%) and release characteristics with entrapment efficiency of 95.2±0.32%. Microspheres fabricated with ethylcellulose to HPMC K4M in the ratio 8.5:1.5 released 98.67% of the entrapped drug in 12 h. Muscle relaxation caused by baclofen microspheres impairs the rotarod performance for more than 12 h. Abdominal X-ray images showed that the gastroretention period of the floating barium sulfate- labeled microspheres was no less than 10 h. The buoyant baclofen microspheres provide a promising gastroretentive drug delivery system to deliver baclofen in spastic patients with a sustained release rate.
Graphical Abstract:
Abdominal x-ray imaging, Baclofen, Central large cavity, Floating sustained release microspheres, Rotarod.
STES's Sinhgad College of Pharmacy, Vadgaon (Bk.), Pune-411041, Maharashtra, India.